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    • 1. 发明申请
    • Progesterone Solutions for Increased Bioavailability
    • 孕激素提高生物利用度的解决方案
    • US20100255085A1
    • 2010-10-07
    • US12752629
    • 2010-04-01
    • Zhi LiuSaujanya L. GosangariDana S. ToopsAqeel Fatmi
    • Zhi LiuSaujanya L. GosangariDana S. ToopsAqeel Fatmi
    • A61K9/48A61K31/57A61P5/34
    • A61K9/4858A61K31/57A61K47/12A61K47/14
    • Fill materials for hydrophobic drugs, such as progesterone, and methods of making and using thereof are described herein. The fill material contains the hydrophobic drug dissolved in one or more fatty acids. The concentration of the hydrophobic drug is typically from about 7% to about 50% by weight of the fill material. The concentration of the one or more fatty acids is from about 60% to about 95% by weight of the carrier. The formulation also contains an organic acid and one or both of one or more pharmaceutically acceptable alcohols and one or more pharmaceutically acceptable mono-, di-, or triesters of medium or long chain fatty acids. The fill material can be encapsulated in a hard or soft capsule. The formulations described herein have a higher dissolution rate and faster onset of dissolution compared to micronized progesterone suspended in an oil and thus should have increased bioavailability in vivo.
    • 本文描述了用于疏水性药物(例如孕酮)的填充材料及其制备和使用方法。 填充材料含有溶解在一种或多种脂肪酸中的疏水性药物。 疏水性药物的浓度通常为填充材料重量的约7%至约50%。 一种或多种脂肪酸的浓度为载体重量的约60%至约95%。 制剂还含有一种有机酸和一种或多种药学上可接受的醇和一种或多种药学上可接受的中,长链脂肪酸的一,二或三酯的一种或两种。 填充材料可以被包封在硬或软胶囊中。 与悬浮在油中的微粉化孕酮相比,本文所述的制剂具有更高的溶解速率和更快的溶解出现,因此应该具有增加的体内生物利用度。
    • 2. 发明授权
    • Progesterone solutions for increased bioavailability
    • 黄体酮提高生物利用度的解决方案
    • US09011908B2
    • 2015-04-21
    • US12752629
    • 2010-04-01
    • Zhi LiuSaujanya L. GosangariDana S. ToopsAqeel Fatmi
    • Zhi LiuSaujanya L. GosangariDana S. ToopsAqeel Fatmi
    • A61P5/34A61K9/48A61K31/57A61K47/12A61K47/14
    • A61K9/4858A61K31/57A61K47/12A61K47/14
    • Fill materials for hydrophobic drugs, such as progesterone, and methods of making and using thereof are described herein. The fill material contains the hydrophobic drug dissolved in one or more fatty acids. The concentration of the hydrophobic drug is typically from about 7% to about 50% by weight of the fill material. The concentration of the one or more fatty acids is from about 60% to about 95% by weight of the carrier. The formulation also contains an organic acid and one or both of one or more pharmaceutically acceptable alcohols and one or more pharmaceutically acceptable mono-, di-, or triesters of medium or long chain fatty acids. The fill material can be encapsulated in a hard or soft capsule. The formulations described herein have a higher dissolution rate and faster onset of dissolution compared to micronized progesterone suspended in an oil and thus should have increased bioavailability in vivo.
    • 本文描述了用于疏水性药物(例如孕酮)的填充材料及其制备和使用方法。 填充材料含有溶解在一种或多种脂肪酸中的疏水性药物。 疏水性药物的浓度通常为填充材料重量的约7%至约50%。 一种或多种脂肪酸的浓度为载体重量的约60%至约95%。 制剂还含有一种有机酸和一种或多种药学上可接受的醇和一种或多种药学上可接受的中,长链脂肪酸的一,二或三酯的一种或两种。 填充材料可以被包封在硬或软胶囊中。 与悬浮在油中的微粉化孕酮相比,本文所述的制剂具有更高的溶解速率和更快的溶解出现,因此应该具有增加的体内生物利用度。
    • 3. 发明授权
    • Stable solutions of orlistat for pharmaceutical dosage forms
    • 用于药物剂型的奥利司他的稳定溶液
    • US08309107B2
    • 2012-11-13
    • US12574215
    • 2009-10-06
    • Zhi LiuDana S. ToopsAqeel A. Fatmi
    • Zhi LiuDana S. ToopsAqeel A. Fatmi
    • A61K9/00A61K9/48A61K31/365A61K31/355A61K31/375
    • A61K9/4858
    • Liquid orlistat-containing fill materials suitable for encapsulating in hard or soft capsules are described herein. The fill material contains orlistat dissolved in one or more medium chain triglycerides or medium chain partial triglycerides, one or more citrate esters, and combinations thereof. The fill material can also contain one or more pharmaceutically acceptable excipients. In one embodiment, the fill material is substantially free of surfactants. The fill material can be encapsulated in hard or soft, gelatin or non-gelatin capsules. The capsules may be coated to modify release of orlistat from the capsule. Alternatively, the fill material can be encapsulated in an enteric capsule, wherein the enteric polymer is a component of the capsule shell, rather than a coating over the capsule shell. The fill materials are stable at elevated temperatures over an extended period of time and allow for high loadings of orlistat (e.g., 20% w/w or higher).
    • 本文描述了适用于包封在硬胶囊或软胶囊中的含有液体奥利司他的填充材料。 填充材料含有溶解在一种或多种中链甘油三酯或中链部分甘油三酸酯中的奥利司他,一种或多种柠檬酸酯及其组合。 填充材料还可以含有一种或多种药学上可接受的赋形剂。 在一个实施方案中,填充材料基本上不含表面活性剂。 填充材料可以包封在硬或软的明胶或非明胶胶囊中。 胶囊可以被涂覆以改变从胶囊释放奥利司他。 或者,填充材料可以包封在肠溶胶囊中,其中肠溶性聚合物是胶囊壳的组分,而不是胶囊壳上的涂层。 填充材料在高温下在延长的时间内是稳定的并且允许高负荷的奥利司他(例如,20%w / w或更高)。
    • 4. 发明申请
    • STABLE SOLUTIONS OF ORLISTAT FOR PHARMACEUTICAL DOSAGE FORMS
    • 用于药物剂型的ORLISTAT的稳定解决方案
    • US20100087520A1
    • 2010-04-08
    • US12574215
    • 2009-10-06
    • Zhi LiuDana S. ToopsAqeel A. Fatmi
    • Zhi LiuDana S. ToopsAqeel A. Fatmi
    • A61K31/365A61K31/355A61K31/375
    • A61K9/4858
    • Liquid orlistat-containing fill materials suitable for encapsulating in hard or soft capsules are described herein. The fill material contains orlistat dissolved in one or more medium chain triglycerides or medium chain partial triglycerides, one or more citrate esters, and combinations thereof. The fill material can also contain one or more pharmaceutically acceptable excipients. In one embodiment, the fill material is substantially free of surfactants. The fill material can be encapsulated in hard or soft, gelatin or non-gelatin capsules. The capsules may be coated to modify release of orlistat from the capsule. Alternatively, the fill material can be encapsulated in an enteric capsule, wherein the enteric polymer is a component of the capsule shell, rather than a coating over the capsule shell. The fill materials are stable at elevated temperatures over an extended period of time and allow for high loadings of orlistat (e.g., 20% w/w or higher).
    • 本文描述了适用于包封在硬胶囊或软胶囊中的含有液体奥利司他的填充材料。 填充材料含有溶解在一种或多种中链甘油三酯或中链部分甘油三酸酯中的奥利司他,一种或多种柠檬酸酯及其组合。 填充材料还可以含有一种或多种药学上可接受的赋形剂。 在一个实施方案中,填充材料基本上不含表面活性剂。 填充材料可以包封在硬或软的明胶或非明胶胶囊中。 胶囊可以被涂覆以改变从胶囊释放奥利司他。 或者,填充材料可以包封在肠溶胶囊中,其中肠溶性聚合物是胶囊壳的组分,而不是胶囊壳上的涂层。 填充材料在高温下在延长的时间内是稳定的并且允许高负荷的奥利司他(例如,20%w / w或更高)。